Evidence map›Paper›PMID 42494118›Full record

ReviewChemical biology & drug design2026

Integrative Insights Into DYRK1A From Molecular Function to Therapeutic Advancement.

Sampriti Paul, Sonal Dubey, Prashant Tiwari

Abstract readReview
In one paragraph

Review in Chemical biology & drug design, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

0 citing papers in PubMed.

No citing paper in PubMed yet.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

3 authors.

Sampriti PaulCollege of Pharmaceutical Sciences, Dayananda Sagar University, Bengaluru South, India.ORCID https://orcid.org/0009-0005-5189-5179
Sonal DubeyCollege of Pharmaceutical Sciences, Dayananda Sagar University, Bengaluru South, India.ORCID https://orcid.org/0000-0003-3073-1173
Prashant TiwariCollege of Pharmaceutical Sciences, Dayananda Sagar University, Bengaluru South, India.ORCID https://orcid.org/0000-0003-4423-6819

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Dual-specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), located within the Down syndrome critical region and implicated in Alzheimer's disease (AD), Parkinson's disease (PD), and context-dependent cancer biology, represents a high-value yet challenging therapeutic target. This review compiles comprehensive structure-activity relationship (SAR) insights essential for medicinal chemists designing selective DYRK1A inhibitors. We detail the molecular architecture of the ATP-binding pocket of DYRK1A, key regulatory residues (Lys188, Phe238, Glu239, Leu241), and structure-function relationships governing inhibitor classes: ATP-competitive agents, ATP-non-competitive inhibitors, and Proteolysis-Targeting Chimeras (PROTAC) degraders with emphasis on functional group modifications and scaffold optimization strategies. Readers will gain actionable insights on binding mode predictions, potency-selectivity trade-offs, and prioritization of lead compounds for preclinical validation. The framework addresses pharmacokinetic property optimization and selectivity profiling across kinase families, enabling researchers to accelerate rational inhibitor design and facilitate translation of DYRK1A therapeutics into clinical trials for neurodegenerative and developmental disorders.

Indexed as

Protein Kinase InhibitorsProtein Serine-Threonine KinasesAdenosine TriphosphateAnimalsBinding SitesDrug DesignDyrk KinasesHumansProtein-Tyrosine KinasesProteolysis Targeting ChimeraStructure-Activity RelationshipTyrosine Kinase InhibitorsAdenosine TriphosphateDyrk KinasesProtein Kinase InhibitorsProtein Serine-Threonine KinasesProtein-Tyrosine KinasesProteolysis Targeting ChimeraTyrosine Kinase InhibitorsAlzheimer diseaseDown syndromeDYRK1Aprotein kinase inhibitorstructure–activity relationship

Identifiers

PMID42494118
PMCPMC13396826

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.